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Fragment-based development of triazole-substituted O-galactosyl aldoximes with fragment-induced affinity and selectivity for galectin-3.

Author

Summary, in English

A fragment-based development of 3C-triazol-1-yl-O-galactopyranosyl aldoximes led to the discovery of highly selective and high affinity (K(d) down to 11 microm) small monosaccharide based inhibitors of galectin-3. Galectin-7, 8 N-terminal CRD, and 9 N-terminal CRD bound the inhibitors only weakly. The galectin-3 selectivity was hypothesized to stem from interaction of the aldoxime moiety with a site not present in the other galectins.

Publishing year

2009

Language

English

Pages

3982-3990

Publication/Series

Organic and Biomolecular Chemistry

Volume

7

Issue

19

Document type

Journal article

Publisher

Royal Society of Chemistry

Topic

  • Immunology in the medical area
  • Microbiology in the medical area

Status

Published

ISBN/ISSN/Other

  • ISSN: 1477-0539